title: Can bioadhesive nanoparticles allow for more effective particle uptake from the small intestine?
abstract: There has been increasing interest in developing bioadhesive nanoparticles due to their great potential as carriers for therapeutics in oral drug delivery systems. Despite decades of research, such a system still has not been successfully implemented. This paper demonstrates the enormous potential of such engineered systems: the incorporation of a bioadhesive coating, poly(butadiene-maleic anhydride-co-L-DOPA) (PBMAD), to non-bioadhesive nanospheres resulted in an enhancement of particle uptake in the small intestine from 5.8±1.9% to 66.9±12.9%. Direct correlation was obtained between bulk tensile strength, in vitro binding to everted intestinal sacs and quantitative in vivo uptake; this data suggests that bulk properties of polymers can be used to predict bioadhesive properties of nano- and microparticles. The differential distribution of the nanospheres to various tissues following uptake suggests surface chemistry plays a significant role in their localization within the body. The results of these studies provide strong support for the use of bioadhesive polymers to enhance nano- and micro-particle uptake from the small intestine for oral drug delivery.
authors.affiliation: Department of Pharmaceutical Sciences, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit MI 48202, USA.
authors.forename: J
authors.initials: J
authors.lastname: Reineke
authors.forename: D Y
authors.initials: DY
authors.lastname: Cho
authors.forename: Y L
authors.initials: YL
authors.lastname: Dingle
authors.forename: P
authors.initials: P
authors.lastname: Cheifetz
authors.forename: B
authors.initials: B
authors.lastname: Laulicht
authors.forename: D
authors.initials: D
authors.lastname: Lavin
authors.forename: S
authors.initials: S
authors.lastname: Furtado
authors.forename: E
authors.initials: E
authors.lastname: Mathiowitz
mesh_terms: D000268:Adhesiveness; D000818:Animals; D007408:Intestinal Absorption; D007583:Jejunum / Q000378:metabolism*; D008297:Male; D008863:Microspheres; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D011108:Polymers / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D011108:Polymers
keywords: Bioadhesion; In-vitro in-vivo correlation; Nanoparticles; Uptake